141283-87-6

141283-87-6 structure

Name: IS-741
Chemical Name: N-[2-(ethylsulfonylamino)-5-(trifluoromethyl)pyridin-3-yl]cyclohexanecarboxamide
CAS Number: 141283-87-6
Molecular Formula: C₁₅H₂₀F₃N₃O₃S
Molecular Weight: 379.39800
Catalog: Signaling Pathways Metabolic Enzyme/Protease Phospholipase
Create Date: 2017-04-08 13:54:01
Modify Date: 2024-01-13 19:13:11
Fuzapladib (IS-741) is a potent phospholipase A2 inhibitor. Fuzapladib can block the adhesion of inflammatory cells to microvascular endothelial cells, inhibit the infiltration of neutrophils into the pancreas or acute pancreatitis, and has anti-acute pancreatitis effects[1].

Name	N-[2-(ethylsulfonylamino)-5-(trifluoromethyl)pyridin-3-yl]cyclohexanecarboxamide
Synonyms	IS 741 N-(2-((Ethylsulfonyl)amino)-5-(trifluoromethyl)-3-pyridinyl)cyclohexanecarboxamide Cyclohexanecarboxamide,N-(2-((ethylsulfonyl)amino)-5-(trifluoromethyl)-3-pyridinyl)

Description	Fuzapladib (IS-741) is a potent phospholipase A2 inhibitor. Fuzapladib can block the adhesion of inflammatory cells to microvascular endothelial cells, inhibit the infiltration of neutrophils into the pancreas or acute pancreatitis, and has anti-acute pancreatitis effects[1].
Related Catalog	Signaling Pathways >> Metabolic Enzyme/Protease >> Phospholipase Research Areas >> Inflammation/Immunology
In Vitro	Fuzapladib(IS-741)(1 μM, 3 h)在脂多糖刺激下，可显着抑制 HL-60 细胞与 HUVEC 的粘附[1]。
In Vivo	Fuzapladib(IS-741)(p.o., 50 mg/kg, 7 days) 显着降低了大鼠回肠中的髓过氧化物酶 (MPO) 活性和粘膜 IL-8 水平，减少了多形核细胞和 Mac-1 阳性细胞向发炎病灶的浸润，有效减轻了三硝基苯磺酸(TNBS)诱导的大鼠回肠炎[2]。
References	[1]. H Shikama, et al. Effect of IS-741 on Cell Adhesion between Human Umbilical Vein Endothelial Cells and HL-60 Cells. [2]. Tetsuya Fukunaga, et al. A novel diamino-pyridine derivative (IS-741) attenuates rat ileitis induced by trinitrobenzene sulfonic acid. J Gastroenterol. 2003;38(5):451-9.